C07F9/65515

ENZYMATIC SYNTHESIS OF 4'-ETHYNYL NUCLEOSIDE ANALOGS

The present invention relates to an enzymatic synthesis of 4′-ethynyl-2′-deoxy nucleosides and analogs thereof, for example EFdA, that eliminates the use of protecting groups on the intermediates, improves the stereoselectivity of glycosylation and reduces the number of process steps needed to make said compounds. It also relates to the novel intermediates employed in the process.

Salts of prodrugs of piperazine and substituted piperidine antiviral agents

This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. ##STR00001##
wherein: X is C or N with the proviso that when X is N, R.sup.1 does not exist; W is C or N with the proviso that when W is N, R.sup.2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of ##STR00002## Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I. ##STR00003##
wherein: L and M are independently selected from the group consisting of C.sub.1-C.sub.6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.

SOLID SUPPORT FOR SYNTHESIZING NUCLEIC ACID SEQUENCES AND METHODS FOR MAKING AND USING

Disclosed herein are embodiments of a solid support suitable for synthesizing nucleic acid sequences. The solid support may have a structure according to Formula I, where CPG is controlled pore glass, and m, n, x, y, R.sup.1 and R.sup.2 are as defined herein.

##STR00001##

Also disclosed are methods for making and using the solid support, kits including solid support, and a universal linker phosphoramidite suitable for use in the solid support.

Antibody-nanoparticle conjugates and methods for making and using such conjugates

Disclosed herein are antibody-nanoparticle conjugates that include two or more nanoparticles (such as gold, palladium, platinum, silver, copper, nickel, cobalt, iridium, or an alloy of two or more thereof) directly linked to an antibody or fragment thereof through a metal-thiol bond. Methods of making the antibody-nanoparticle conjugates disclosed herein include reacting an arylphosphine-nanoparticle composite with a reduced antibody to produce an antibody-nanoparticle conjugate. Also disclosed herein are methods for detecting a target molecule in a sample that include using an antibody-nanoparticle conjugate (such as the antibody-nanoparticle conjugates described herein) and kits for detecting target molecules utilizing the methods disclosed herein.

Stabilized Polyolefin Compositions Comprising Benzofuranones and Hindered Phenolic Antioxidants
20220145053 · 2022-05-12 ·

Polyolefin compositions comprising i) a polyolefin, ii) one or more phosphorus-containing benzofuranone compounds and iii) one or more hindered phenolic antioxidants are provided excellent protection against discoloration and enhanced thermal stability during melt processing as exhibited by improved retention of molecular weight and maintenance of polymer molecular architecture.

Derivatives of korormicin useful as antibiotics
11324716 · 2022-05-10 ·

Described herein is a process for antibiotic development comprising: (a) generating a compound of formula (III): ##STR00001##
or a salt or stereoisomer or prodrug thereof; wherein R.sup.1-R.sup.3 and R.sup.5-R.sup.10 are independently selected from H, alkyl group, substituted alkyl group, halogen, OH, NH.sub.2, or SH; R.sup.4 is H, alkyl group or substituted alkyl group; X.sup.1-X.sup.2 are independently selected from ═O, ═S, ═NH, H, alkyl, halogen, OH, SH, or NH.sub.2; W is a saturated acyclic hydrocarbon chain of 1 to 15 carbon atoms; and Z is a neutral or positively charged organic group comprising a nitrogen or phosphorus atom; and; and (b) determining efficacy of the compound to inhibit growth of a bacteria. Systems of drug development of these antibiotic compounds are also described.

NUCLEOTIDE CLEAVABLE LINKERS AND USES THEREOF

Disclosed herein, inter alia, are compounds, compositions, and methods of use thereof for sequencing a nucleic acid.

BIOINSPIRED LIPID DERIVATIVES AND USES THEREOF
20230303598 · 2023-09-28 ·

The present disclosure relates to compounds, compositions, and methods for delivery of therapeutic, diagnostic, or prophylactic agents (for example, a nucleic acid).

Arabitol and xylitol based flame retardants

A flame retardant sugar-derived molecule, a process for forming a flame retardant sugar-derived molecule, and an article of manufacture comprising a flame retardant sugar-derived molecule are disclosed. The flame retardant sugar-derived molecule can be synthesized from arabitol, xylitol, arabic acid, or xylonic acid obtained from a bio-based source, and can have at least one phosphoryl or phosphonyl moiety. The process for forming the flame retardant sugar-derived molecule can include reacting arabitol, xylitol, arabic acid, or xylonic acid and a flame retardant phosphorus-based molecule to form the flame retardant sugar-derived molecule.

PHOSPHORAMIDATE DERIVATIVES OF 5 - FLUORO - 2` - DEOXYURIDINE FOR USE IN THE TREATMENT OF CANCER

Phosphoramidate derivatives of 5-fluoro-2′-deoxyuridine are disclosed for use in the treatment of cancer, especially in the treatment of cancer where the patient shows resistance, for example, in a patient with cells with a lowered level of nucleoside transporter proteins and/or with nucleoside kinase-deficient cells and/or with Mycoplasma-infected cells and/or with cells with a raised level of thymidylate synthase.